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Items: 1 to 50 of 85

1.

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.

Burke JR, Cheng L, Gillooly KM, Strnad J, Zupa-Fernandez A, Catlett IM, Zhang Y, Heimrich EM, McIntyre KW, Cunningham MD, Carman JA, Zhou X, Banas D, Chaudhry C, Li S, D'Arienzo C, Chimalakonda A, Yang X, Xie JH, Pang J, Zhao Q, Rose SM, Huang J, Moslin RM, Wrobleski ST, Weinstein DS, Salter-Cid LM.

Sci Transl Med. 2019 Jul 24;11(502). pii: eaaw1736. doi: 10.1126/scitranslmed.aaw1736.

PMID:
31341059
2.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.

J Med Chem. 2019 Jul 18. doi: 10.1021/acs.jmedchem.9b00444. [Epub ahead of print]

PMID:
31318208
3.

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS.

J Med Chem. 2019 Jul 17. doi: 10.1021/acs.jmedchem.9b00443. [Epub ahead of print]

PMID:
31314518
4.

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).

Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29.

PMID:
30893553
5.

Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.

Liu C, Lin J, Moslin R, Tokarski JS, Muckelbauer J, Chang C, Tredup J, Xie D, Park H, Li P, Wu DR, Strnad J, Zupa-Fernandez A, Cheng L, Chaudhry C, Chen J, Chen C, Sun H, Elzinga P, D'arienzo C, Gillooly K, Taylor TL, McIntyre KW, Salter-Cid L, Lombardo LJ, Carter PH, Aranibar N, Burke JR, Weinstein DS.

ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. doi: 10.1021/acsmedchemlett.9b00035. eCollection 2019 Mar 14.

PMID:
30891145
6.

Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Spergel SH, Mertzman ME, Kempson J, Guo J, Stachura S, Haque L, Lippy JS, Zhang RF, Galella M, Pitt S, Shen G, Fura A, Gillooly K, McIntyre KW, Tang V, Tokarski J, Sack JS, Khan J, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Schieven GL, Wrobleski ST, Pitts WJ.

ACS Med Chem Lett. 2019 Feb 13;10(3):306-311. doi: 10.1021/acsmedchemlett.8b00508. eCollection 2019 Mar 14.

PMID:
30891131
7.

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials.

Gilmore JL, Xiao HY, Dhar TGM, Yang MG, Xiao Z, Xie J, Lehman-McKeeman LD, Gong L, Sun H, Lecureux L, Chen C, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Borowski V, Warrack BM, Li Y, Shi H, Levesque PC, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Rampulla R, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Salter-Cid LM, Carter PH, Dyckman AJ.

J Med Chem. 2019 Mar 14;62(5):2265-2285. doi: 10.1021/acs.jmedchem.8b01695. Epub 2019 Mar 6.

PMID:
30785748
8.

Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care.

Gillooly KM, Pulicicchio C, Pattoli MA, Cheng L, Skala S, Heimrich EM, McIntyre KW, Taylor TL, Kukral DW, Dudhgaonkar S, Nagar J, Banas D, Watterson SH, Tino JA, Fura A, Burke JR.

PLoS One. 2017 Jul 24;12(7):e0181782. doi: 10.1371/journal.pone.0181782. eCollection 2017.

9.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.

J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5.

PMID:
28541707
10.

Selective IRAK4 Inhibition Attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity.

Dudhgaonkar S, Ranade S, Nagar J, Subramani S, Prasad DS, Karunanithi P, Srivastava R, Venkatesh K, Selvam S, Krishnamurthy P, Mariappan TT, Saxena A, Fan L, Stetsko DK, Holloway DA, Li X, Zhu J, Yang WP, Ruepp S, Nair S, Santella J, Duncia J, Hynes J, McIntyre KW, Carman JA.

J Immunol. 2017 Feb 1;198(3):1308-1319. doi: 10.4049/jimmunol.1600583. Epub 2016 Dec 21.

11.

Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.

Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7.

PMID:
28002964
12.

Identification of potent tricyclic prodrug S1P1 receptor modulators.

Marcoux D, Xiao HY, Murali Dhar TG, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Shi H, Levesque PC, Sun H, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Gupta A, Pragalathan B, Rampulla R, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Lombardo LJ, Carter PH, Dyckman AJ.

Medchemcomm. 2016 Nov 25;8(4):725-729. doi: 10.1039/c6md00539j. eCollection 2017 Apr 1.

13.

Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.

Xiao HY, Watterson SH, Langevine CM, Srivastava AS, Ko SS, Zhang Y, Cherney RJ, Guo WW, Gilmore JL, Sheppeck JE 2nd, Wu DR, Li P, Ramasamy D, Arunachalam P, Mathur A, Taylor TL, Shuster DJ, McIntyre KW, Shen DR, Yarde M, Cvijic ME, Marino AM, Balimane PV, Yang Z, Banas DM, Cornelius G, D'Arienzo CJ, Warrack BM, Lehman-McKeeman L, Salter-Cid LM, Xie J, Barrish JC, Carter PH, Dyckman AJ, Dhar TG.

J Med Chem. 2016 Nov 10;59(21):9837-9854. Epub 2016 Oct 20.

PMID:
27726358
14.

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.

Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2016 Oct 13;59(19):9173-9200. Epub 2016 Sep 19.

PMID:
27583770
15.

Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).

De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA.

J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26.

PMID:
27531604
16.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.

J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1.

PMID:
27309907
17.

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).

Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1.

PMID:
27055941
18.

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

Dhar TG, Xiao HY, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Warrack B, Shi H, Levesque PC, Zhu JL, Hennan J, Balimane P, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

ACS Med Chem Lett. 2016 Jan 19;7(3):283-8. doi: 10.1021/acsmedchemlett.5b00448. eCollection 2016 Mar 10.

19.

Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.

Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10.

PMID:
26924461
20.

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

Liu C, Lin J, Hynes J, Wu H, Wrobleski ST, Lin S, Dhar TG, Vrudhula VM, Sun JH, Chao S, Zhao R, Wang B, Chen BC, Everlof G, Gesenberg C, Zhang H, Marathe PH, McIntyre KW, Taylor TL, Gillooly K, Shuster DJ, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2015 Oct 8;58(19):7775-84. doi: 10.1021/acs.jmedchem.5b00839. Epub 2015 Sep 22.

PMID:
26359680
21.

Dual Inhibition of Interleukin-23 and Interleukin-17 Offers Superior Efficacy in Mouse Models of Autoimmunity.

Mangan PR, Su LJ, Jenny V, Tatum AL, Picarillo C, Skala S, Ditto N, Lin Z, Yang X, Cotter PZ, Shuster DJ, Song Y, Borowski V, Thomas RL, Heimrich EM, Devaux B, Das Gupta R, Carvajal I, McIntyre KW, Xie J, Zhao Q, Struthers M, Salter-Cid LM.

J Pharmacol Exp Ther. 2015 Aug;354(2):152-65. doi: 10.1124/jpet.115.224246. Epub 2015 May 26.

PMID:
26015463
22.

Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H-pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341).

Yang MG, Dhar TG, Xiao Z, Xiao HY, Duan JJ, Jiang B, Galella MA, Cunningham M, Wang J, Habte S, Shuster D, McIntyre KW, Carman J, Holloway DA, Somerville JE, Nadler SG, Salter-Cid L, Barrish JC, Weinstein DS.

J Med Chem. 2015 May 28;58(10):4278-90. doi: 10.1021/acs.jmedchem.5b00257. Epub 2015 May 7.

PMID:
25905990
23.

Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.

Shi Q, Tebben A, Dyckman AJ, Li H, Liu C, Lin J, Spergel S, Burke JR, McIntyre KW, Olini GC, Strnad J, Surti N, Muckelbauer JK, Chang C, An Y, Cheng L, Ruan Q, Leftheris K, Carter PH, Tino J, De Lucca GV.

Bioorg Med Chem Lett. 2014 May 1;24(9):2206-11. doi: 10.1016/j.bmcl.2014.02.075. Epub 2014 Mar 13.

PMID:
24685542
24.

Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5.

PMID:
22018461
25.

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.

Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV.

Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21.

PMID:
22015772
26.

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.

Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. doi: 10.1016/j.bmcl.2011.05.091. Epub 2011 May 30.

PMID:
21705217
27.

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.

Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31.

PMID:
21087862
28.

5-amino-pyrazoles as potent and selective p38α inhibitors.

Das J, Moquin RV, Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Newitt JA, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6886-9. doi: 10.1016/j.bmcl.2010.10.034. Epub 2010 Oct 13.

PMID:
21035336
29.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM, Pitt S, Shen DR, Zhang RF, McIntyre KW, Salter-Cid L, Shuster DJ, Zhang H, Marathe PH, Doweyko AM, Sack JS, Kiefer SE, Kish KF, Newitt JA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2010 Sep 23;53(18):6629-39. doi: 10.1021/jm100540x.

PMID:
20804198
30.

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG.

J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u.

PMID:
20405922
31.

An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis.

Suchard SJ, Stetsko DK, Davis PM, Skala S, Potin D, Launay M, Dhar TG, Barrish JC, Susulic V, Shuster DJ, McIntyre KW, McKinnon M, Salter-Cid L.

J Immunol. 2010 Apr 1;184(7):3917-26. doi: 10.4049/jimmunol.0901095. Epub 2010 Feb 26.

32.

Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis.

Gillooly KM, Pattoli MA, Taylor TL, Chen L, Cheng L, Gregor KR, Whitney GS, Susulic V, Watterson SH, Kempson J, Pitts WJ, Booth-Lute H, Yang G, Davies P, Kukral DW, Strnad J, McIntyre KW, Darienzo CJ, Salter-Cid L, Yang Z, Wang-Iverson DB, Burke JR.

J Pharmacol Exp Ther. 2009 Nov;331(2):349-60. doi: 10.1124/jpet.109.156018. Epub 2009 Aug 3.

PMID:
19652024
33.

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

Bioorg Med Chem Lett. 2009 May 15;19(10):2646-9. doi: 10.1016/j.bmcl.2009.03.159. Epub 2009 Apr 5.

PMID:
19376699
34.

Novel tricyclic inhibitors of IkappaB kinase.

Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816.

PMID:
19267461
35.

A structured light-based system for scanning subcutaneous tumors in laboratory animals.

Girit IC, Jure-Kunkel M, McIntyre KW.

Comp Med. 2008 Jun;58(3):264-70.

36.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

Wrobleski ST, Lin S, Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M, Dodd J, Barrish JC, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2739-44. doi: 10.1016/j.bmcl.2008.02.067. Epub 2008 Mar 4.

PMID:
18364256
37.

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2652-7. doi: 10.1016/j.bmcl.2008.03.019. Epub 2008 Mar 10.

PMID:
18359226
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The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. doi: 10.1016/j.bmcl.2008.02.031. Epub 2008 Feb 16.

PMID:
18313298
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Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

Hynes J Jr, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K.

J Med Chem. 2008 Jan 10;51(1):4-16. Epub 2007 Dec 12.

PMID:
18072718
40.

Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).

Watterson SH, Chen P, Zhao Y, Gu HH, Dhar TG, Xiao Z, Ballentine SK, Shen Z, Fleener CA, Rouleau KA, Obermeier M, Yang Z, McIntyre KW, Shuster DJ, Witmer M, Dambach D, Chao S, Mathur A, Chen BC, Barrish JC, Robl JA, Townsend R, Iwanowicz EJ.

J Med Chem. 2007 Jul 26;50(15):3730-42. Epub 2007 Jun 22.

PMID:
17585753
41.

Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.

Belema M, Bunker A, Nguyen VN, Beaulieu F, Ouellet C, Qiu Y, Zhang Y, Martel A, Burke JR, McIntyre KW, Pattoli MA, Daloisio C, Gillooly KM, Clarke WJ, Brassil PJ, Zusi FC, Vyas DM.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. Epub 2007 May 16.

PMID:
17540562
42.

Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.

Beaulieu F, Ouellet C, Ruediger EH, Belema M, Qiu Y, Yang X, Banville J, Burke JR, Gregor KR, MacMaster JF, Martel A, McIntyre KW, Pattoli MA, Zusi FC, Vyas D.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1233-7. Epub 2006 Dec 9.

PMID:
17197177
43.

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.

Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC.

J Med Chem. 2006 Nov 16;49(23):6819-32.

PMID:
17154512
44.

Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

Potin D, Launay M, Monatlik F, Malabre P, Fabreguettes M, Fouquet A, Maillet M, Nicolai E, Dorgeret L, Chevallier F, Besse D, Dufort M, Caussade F, Ahmad SZ, Stetsko DK, Skala S, Davis PM, Balimane P, Patel K, Yang Z, Marathe P, Postelneck J, Townsend RM, Goldfarb V, Sheriff S, Einspahr H, Kish K, Malley MF, DiMarco JD, Gougoutas JZ, Kadiyala P, Cheney DL, Tejwani RW, Murphy DK, Mcintyre KW, Yang X, Chao S, Leith L, Xiao Z, Mathur A, Chen BC, Wu DR, Traeger SC, McKinnon M, Barrish JC, Robl JA, Iwanowicz EJ, Suchard SJ, Dhar TG.

J Med Chem. 2006 Nov 30;49(24):6946-9.

PMID:
17125246
45.

Core exploration in optimization of chemokine receptor CCR4 antagonists.

Purandare AV, Wan H, Somerville JE, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):679-82. Epub 2006 Nov 2.

PMID:
17098428
46.

A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice.

Kang L, McIntyre KW, Gillooly KM, Yang Y, Haycock J, Roberts S, Khanna A, Herpin TF, Yu G, Wu X, Morton GC, Tuerdi H, Koplowitz B, Walker SG, Wardwell-Swanson J, Macor JE, Lawrence RM, Carlson KE.

J Leukoc Biol. 2006 Oct;80(4):897-904. Epub 2006 Aug 3.

PMID:
16888084
47.

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Das J, Furch JA, Liu C, Moquin RV, Lin J, Spergel SH, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Doweyko AM, Kamath A, Zhang H, Marathe P, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3706-12. Epub 2006 May 6.

PMID:
16682193
48.

Selective inhibition of eosinophil influx into the lung by small molecule CC chemokine receptor 3 antagonists in mouse models of allergic inflammation.

Das AM, Vaddi KG, Solomon KA, Krauthauser C, Jiang X, McIntyre KW, Yang XX, Wadman E, Welch P, Covington M, Graden D, Yeleswaram K, Trzaskos JM, Newton RC, Mandlekar S, Ko SS, Carter PH, Davies P.

J Pharmacol Exp Ther. 2006 Jul;318(1):411-7. Epub 2006 Apr 13.

PMID:
16614169
49.

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

Das J, Liu C, Moquin RV, Lin J, Furch JA, Spergel SH, Doweyko AM, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.

Bioorg Med Chem Lett. 2006 May 1;16(9):2411-5. Epub 2006 Feb 14. Erratum in: Bioorg Med Chem Lett. 2006 Aug 1;16(15):4148. Doweyko, Arthur M [added].

PMID:
16481166
50.

Optimization of CCR4 antagonists: side-chain exploration.

Purandare AV, Wan H, Gao A, Somerville J, Burke C, Vaccaro W, Yang X, McIntyre KW, Poss MA.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):204-7. Epub 2005 Oct 19.

PMID:
16236499

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